INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES Russian patent published in 2018 - IPC C07D405/14 C07D413/14 C07D401/04 C07D403/04 C07D413/04 C07D487/04 C07D498/04 C07D417/04 C07D471/04 A61K31/4409 A61K31/4406 A61K31/4402 A61P25/00 

FIELD: medicine.

SUBSTANCE: invention relates to 2-oxo-2,3-dihydroindoles of general formula (I), wherein Ar is a 6-membered heteroaryl group containing one or two N atoms, which is a pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms selected from N, S or O, which is imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; R¹ is a hydrogen atom, C_1-7-alkyl, halogen atom, amino, dimethylamino, cyano, C_1-7-alkyl substituted with a halogen atom, C_1-7-alkyl substituted with hydroxy, CH(OH)CF₃, (CH₂)_o-C_1-7-alkoxy, C_3-6cycloalkyl optionally substituted with CF₃, or a heterocycloalkyl selected from pyrrolidinyl, morpholinyl, piperazinyl, tetrahydropyran-4-yl and oxetanyl, optionally substituted with C_1-7-alkyl; R² is a hydrogen atom, C_1-7-alkyl, (CH₂)_o-C_3-6-cycloalkyl, (CH₂)_o-OC_3-6-cycloalkyl, (CH₂)_o-C_1-7-alkoxy, (CH₂)_o-C_1-7-alkoxy substituted with a halogen atom, (CH₂)_o-heterocycloalkyl, selected from tetrahydrofuran-3-yl, oxetanyl, optionally substituted C_1-7-alkyl, and tetrahydrofuran-2-yl substituted with hydroxy group and hydroxy-C_1-7-alkyl, (CH₂)_o-S(O)₂-C_3-6-cycloalkyl, C_1-7-alkyl substituted with one or two hydroxy groups, C_1-7-alkyl substituted with one or two C_1-7-alkoxy, (CH₂)_o-S(O)₂-C_1-7-alkyl, C_1-7-alkyl, substituted with a halogen atom, or CH₂CH (OH) CF₃; R³ is a halogen atom or C_1-7-alkyl; X is CH or N; X¹ is CH or N; n equals 1 or 2; o is 0, 1, 2, or 3; m is 0, 1 or 2; and the dotted line represents a link or its absence; as well as pharmaceutically acceptable salts, stereoisomers, enantiomers or a racemic mixture thereof. .

EFFECT: compounds can be used to treat certain disorders of the central nervous system, which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, addiction to alcohol and medical drugs, obsessive-compulsive disorder, cognitive impairment, bipolar disorder, mood disorders, major depression, depression, resistant to treatment, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disorders, chronic fatigue syndrome, stiffness, with anti-inflammatory effects in arthritis and balance disorders.

23 cl, 2 dwg, 5 tbl, 176 ex